IP Library Granted Patent US 11,261,205
Granted Patent B2
US 11,261,205 · App. 16/908,244 · Granted Mar 1, 2022

Oxazolidinone-quinolone hybrid antibacterial for the parenteral treatment of prophylaxis of bacterial diseases

Inventors: Thomas Kapsner (Gröbenzell, DE); Axel Dalhoff (Wuppertal, DE); Thomas Gramatte (Dresden, DE)
Assignee: Morphochem GmbH
C07F9/653A61K31/4375A61K31/4709A61P1/00A61P1/12A61P31/00A61P31/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,261,205
App. No.
16/908,244
Granted
Mar 1, 2022
Kind
B2
Abstract

The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.

Claims (22)

1. A method for treating a bacterial infection caused by Clostridium difficile , comprising administering to a patient in need thereof a compound, which is 7-(4-{4-[(5S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2-fluoro-phenoxymethyl}-4-phosphonooxy-piperidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid:

or a pharmacologically acceptable salt thereof.

2. The method according to claim 1 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered by an infusion.

3. The method according to claim 2 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered at an infusion rate of from 0.4 to 3 mg/(kg body weight×h).

4. The method according to claim 3 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered at an infusion rate of from 0.4 to 1.5 mg/(kg body weight×h).

5. The method according to claim 4 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered at an infusion rate of from 0.4 to 0.75 mg/(kg body weight×h).

6. The method according to claim 5 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered at an infusion rate of 0.5 mg/(kg body weight×h).

7. The method according to claim 1 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered over a period of from 20 min to 24 h per day.

8. The method according to claim 7 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered over a period of from 4 h to 12 h per day.

9. The method according to claim 8 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered over a period of 12 h per day.

10. The method according to claim 1 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered daily for a period of up to 10 days.

11. The method according to claim 10 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered daily for a period of 10 days.

12. The method according to claim 1 , wherein the compound, or a pharmacologically acceptable salt thereof, is administered daily at a dose of 6 mg/kg.

13. The method according to claim 1 , wherein the compound, or a pharmacologically acceptable salt thereof, is a sodium salt of the compound.

14. The method according to claim 1 , wherein the bacterial infection caused by Clostridium difficile is an intestinal disease caused by Clostridium difficile.

15. The method according to claim 14 , wherein the intestinal disease caused by Clostridium difficile is diarrhea, colitis, or pseudomembranous colitis.

16. The method according to claim 1 , wherein the bacterial infection caused by Clostridium difficile is ileus, toxic megacolon, fulminant colitis, colonic perforation or need for colectomy.

17. A method for treating an intestinal disease caused by Clostridium difficile , comprising administering to a patient in need thereof a compound, which is 7-(4-{4-[(5S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2-fluoro-phenoxymethyl}-4-phosphonooxy-piperidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid:

or a pharmacologically acceptable salt thereof, wherein the compound, or a pharmacologically acceptable salt thereof, is administered daily at an infusion rate of 0.5 mg/(kg body weight×h) over a period of 12 h per day for a period of 10 days.

18. The method according to claim 17 , wherein the intestinal disease caused by Clostridium difficile is diarrhea, colitis, or pseudomembranous colitis.

19. The method according to claim 17 , wherein the intestinal disease caused by Clostridium difficile is ileus, toxic megacolon, fulminant colitis, colonic perforation or need for colectomy.

20. The method according to claim 17 , wherein the compound, or a pharmacologically acceptable salt thereof, is a sodium salt of the compound.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 30, 2020
From: DALHOFF, AXEL; GRAMATTE, THOMAS; KAPSNER, THOMAS
To: MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE
Reel/Frame 053933/0030 →
CHANGE OF NAME Recorded Jun 26, 2020
From: MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE
To: MORPHOCHEM GMBH
Reel/Frame 053066/0695 →
Priority Claims (3)
EP 13002762 · May 28, 2013 · regional
EP 13005745 · Dec 10, 2013 · regional
EP 13005748 · Dec 10, 2013 · regional
Continuity (2)
Continuation 14894400
Related Publication 20200392168A1 · Dec 17, 2020